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Estradiol, mainly as esters including estradiol valerate, estradiol cypionate, and estradiol enanthate, is also the exclusive estrogen used in combined injectable contraceptives. [ 6 ] As of 2021, more than 95% of prescriptions are for combined hormonal birth control forms containing the synthetic estrogen ethinylestradiol (EE). [ 7 ]
Estradiol levels after a short intravenous infusion of 20 mg estradiol in aqueous solution or an intramuscular injection of an equimolar dose of estradiol benzoate, estradiol valerate, or estradiol undecylate in oil solution in women. [6] [7] Sources: Geppert (1975) and Leyendecker et al. (1975). [6] [7]
[1] [10] It has been said that, via intramuscular injection, the duration of estradiol benzoate (with an ester of length 1 carbon plus a benzene ring) is 2 to 3 days, of estradiol dipropionate (with two esters each of length 2 carbons) is 1 to 2 weeks, of estradiol valerate (ester of 5 carbons) is 1 to 3 weeks, and of estradiol cypionate (ester ...
Estradiol plus the fatty acid valeric acid (valerate) equals estradiol valerate, a C17β ester of estradiol. [107] Estradiol valerate is a synthetic estrane steroid and the C17β valerate (pentanoate) fatty acid ester of estradiol. [23] [24] It is also known as estradiol 17β-valerate or as estra-1,3,5(10)-triene-3,17β-diol 17β-pentanoate.
Estradiol cypionate (Depo-Estradiol, Estradiol Cypionate) – 5 mg/mL (1 mg/mL and 3 mg/mL discontinued) Estradiol valerate (Delestrogen, Estradiol Valerate) – 10 mg/mL, 20 mg/mL, 40 mg/mL; Polyestradiol phosphate (Estradurin) was previously available in the U.S. but was discontinued.
Estradiol cypionate is and has been available as an oil solution for intramuscular injection provided in vials and ampoules at concentrations of 1, 3, and 5 mg/mL (and containing 5, 10, 15, 25, or 50 mg estradiol cypionate total).
Estradiol valerate/megestrol acetate; Estradiol valerate/methenmadinone caproate (Lutofollin) Polyestradiol phosphate/medroxyprogesterone acetate; Additional preparations listed at Combined injectable birth control § Research; For other indications: Estradiol valerate/gestonorone caproate (SH-834, SH-8.0834)
Estradiol valerate: 10–40 mg 1x/1–2 weeks Estradiol undecylate: 100 mg 1x/4 weeks Polyestradiol phosphate: Alone: 160–320 mg 1x/4 weeks With oral EE: 40–80 mg 1x/4 weeks Estrone: 2–4 mg 2–3x/week IV injection: Fosfestrol: 300–1200 mg 1–7x/week Estramustine phosphate: 240–450 mg/day Note: Dosages are not necessarily equivalent ...
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